Design and synthesis of 1,5-diarylbenzimidazoles as inhibitors of the VEGF-receptor KDR

被引：15

作者：

Bilodeau, MT ^{[1
]}

Cunningham, AM ^{[1
]}

Koester, TJ ^{[1
]}

Ciecko, PA ^{[1
]}

Coll, KE ^{[1
]}

Huckle, WR ^{[1
]}

Hungate, RW ^{[1
]}

Kendall, RL ^{[1
]}

McFall, RC ^{[1
]}

Mao, XZ ^{[1
]}

Rutledge, RZ ^{[1
]}

Thomas, KA ^{[1
]}

机构：

[1] Merck Res Labs, Dept Med Chem & Canc Res, West Point, PA 19486 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2003年 / 13卷 / 15期

关键词：

D O I：

10.1016/S0960-894X(03)00485-2

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

1, 5-Diarylbenzimidazoles have been identified as potent inhibitors of KDR kinase activity. The series was developed with a goal of finding compounds with optimal drug-like properties. This communication describes structural modifications in the series that enhance solubility, lower protein binding, and provide compounds with excellent potency and pharmacokinetic profiles. (C) 2003 Elsevier Ltd. All rights reserved.

引用

页码：2485 / 2488

页数：4

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